BMS-P5
BMS-P5 Basic information
- Product Name:
- BMS-P5
- Synonyms:
-
- BMS-P5
- Methanone, [(2S,5R)-5-amino-2-methyl-1-piperidinyl][2-[1-(cyclopropylmethyl)-1H-pyrrolo[2,3-b]pyridin-2-yl]-7-methoxy-1-methyl-1H-benzimidazol-5-yl]-
- BMS-P5 free base
- BMS-P-5 free base,BMS P5 free base,myeloma,Inhibitor,inhibit,Protein Arginine Deiminase,BMS-P5,Multiple,NET,BMSP5 free base,Peptidylarginine Deiminase
- ((2S,5R)-5-Amino-2-methylpiperidin-1-yl)(2-(1-(cyclopropylmethyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone
- (2S,5R)-5-amino-2-methyl-1-piperidinyl][2-[1-(cyclopropylmethyl)-1H-pyrrolo[2,3-b]pyridin-2-yl]-7-methoxy-1-methyl-1H-methanone
- BMS-P5 free base, 10 mM in DMSO
- BMS-P5 ，S9644
- CAS:
- 1550371-22-6
- MF:
- C27H32N6O2
- MW:
- 472.58
- Mol File:
- 1550371-22-6.mol
BMS-P5 Chemical Properties
- Boiling point:
- 728.7±70.0 °C(Predicted)
- Density
- 1.40±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMF: 20 mg/ml,DMSO: 5 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:8): 0.11 mg/ml
- form
- A crystalline solid
- pka
- 9.87±0.40(Predicted)
- color
- White to off-white
BMS-P5 Usage And Synthesis
Uses
BMS-P5 free base is a selective and orally active peptidylarginine deiminase 4 (PAD4) inhibitor with an IC50 of 98 nM. BMS-P5 free base shows selective for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 free base blocks multiple myeloma (MM)-induced neutrophil extracellular trap (NET) formation and delays progression of MM in a syngeneic mouse model[1].
in vivo
BMS-P5 (50 mg/kg, oral gavage) significantly improves survival of MM-bearing mice[1].
BMS-P5 (50 mg/kg, oral gavage) may attenuate the presence of pro-tumorigenic proteins in the tumor microenvironment, and thus delay tumor progression[1].
| Animal Model: | Syngeneic mouse model of MM[1]. |
| Dosage: | 50 mg/kg. |
| Administration: | Oral gavage, twice a day beginning on day 3 after tumor cell injection. |
| Result: | Significantly delayed development of symptoms and significantly prolonged survival of MM-bearing mice. |
References
[1] Marina Li, et al. A Novel Peptidylarginine Deiminase 4 (PAD4) Inhibitor BMS-P5 Blocks Formation of Neutrophil Extracellular Traps and Delays Progression of Multiple Myeloma. Mol Cancer Ther. 2020 Jul;19(7):1530-1538. DOI:10.1158/1535-7163.MCT-19-1020
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